Please use this identifier to cite or link to this item: http://hdl.handle.net/2440/105974
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dc.contributor.authorXiao, T.en
dc.contributor.authorLiu, R.en
dc.contributor.authorProud, C.en
dc.contributor.authorWang, M.en
dc.date.issued2016en
dc.identifier.citationActa Pharmaceutica Sinica B, 2016; 6(6):557-563en
dc.identifier.issn2211-3835en
dc.identifier.issn2211-3843en
dc.identifier.urihttp://hdl.handle.net/2440/105974-
dc.description.abstractEukaryotic elongation factor 2 kinase (eEF2K) inhibitors may aid in the development of new therapeutic agents to combat cancer. Purified human eEF2K was obtained from an Escherichia coli expression system and a luminescence-based high-throughput screening (HTS) assay was developed using MH-1 peptide as the substrate. The luminescent readouts correlated with the amount of adenosine triphosphate remaining in the kinase reaction. This method was applied to a large-scale screening campaign against a diverse compound library and subsequent confirmation studies. Nine initial hits showing inhibitory activities on eEF2K were identified from 56,000 synthetic compounds during the HTS campaign, of which, five were chosen to test their effects in cancer cell lines.en
dc.description.statementofresponsibilityTing Xiao, Rui Liu, Christopher G.Proud, Ming-Wei Wangen
dc.language.isoenen
dc.publisherElsevieren
dc.rights© 2016 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).en
dc.subjectHigh-throughput screening; Inhibitors; Luminescence; MH-1 peptide; eEF2Ken
dc.titleA high-throughput screening assay for eukaryotic elongation factor 2 kinase inhibitorsen
dc.typeJournal articleen
dc.identifier.rmid0030060409en
dc.identifier.doi10.1016/j.apsb.2016.04.002en
dc.identifier.pubid277825-
pubs.library.collectionPharmacology publicationsen
pubs.library.teamDS10en
pubs.verification-statusVerifieden
pubs.publication-statusPublisheden
dc.identifier.orcidProud, C. [0000-0003-0704-6442]en
Appears in Collections:Pharmacology publications

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